New c-glycosylpolyphenol antidiabetic agents, effect on glucose tolerance and interaction with beta-amyloid. therapeutic applications of the synthesized agent(s) and of genista tenera ethyl acetate extracts containing some of those agents

Abstract

The present invention concerns the antidiabetic activity of compounds type A, namely of 8-β-D-glucosylgenistein, which is not toxic to eukaryotic cells and has demonstrated to produce complete normalization of fasting hyperglycaemia, to reduce excessive postprandial glucose excursion, to increase glucose-induced insulin secretion and insulin sensitivity. An alternative synthesis for this molecular entity and its binding ability to β-amyloid oligomers is also included in the present invention, which also comprises Genista tenera ethyl acetate extract for use as antihyperglycaemic agent i.e. for lowering blood glucose levels in mammals that are pre-diabetic or have type 2 or type 1 diabetes. The inhibitory activity of β-glucosidase by Genista tenera ethyl acetate and butanol extracts and that of glucose-6-phosphastase by these two extracts and the diethyl ether plant extract is also part of the present invention.

1 . A flavonoid composition consisting essentially of  Genista tenera  characterized by the fact that effective composition is obtained from the aerial parts of the plant and the extraction is performed with ethyl acetate. 
     
     
         2 . A flavonoid composition of  claim 1  wherein the composition is for use as a medicament and/or a nutraceutic or functional food ingredient. 
     
     
         3 . A flavonoid composition according to  claim 2 , wherein the composition is used for treating diabetes. 
     
     
         4 . A flavonoid composition according to  claim 3 , wherein the composition is administered in an amount of 60 milligrams per kilogram body weight per day, for seven days, to a mammal model. 
     
     
         5 . Use of the flavonoid effective composition according to  claim 1  for the preparation of a medicament for the treatment one or more of diabetes, characterized in that the extract is administered intraperitoneally in a dose of 60 mg/Kg of body weight. 
     
     
         6 . A pharmaceutical composition comprising the flavonoid effective composition of  claim 1  that normalizes blood glucose levels on the oral glucose tolerance test (OGTT). 
     
     
         7 . A pharmaceutical preparation in dosage unit form adapted for administration to obtain a therapeutic effect, comprising, per dosage unit, a therapeutically effective amount of the flavonoid composition of  claim 1 . 
     
     
         8 . Medical use of the plant extract of  claim 1 , for treatment of diabetes, wherein a dose of 60 mg/kg of body weight is administered. 
     
     
         9 . A method for treatment of diabetes comprising the step of administering a quantity of a flavonoid effective composition consisting essentially of  Genista tenera,  to result in a reduction of hyperglycaemia. 
     
     
         10 . A pharmaceutical composition comprising ethyl acetate and n-butanol extracts from  Genista tenera  that inhibit the enzyme α-glucosidase, normalizing glucose levels. 
     
     
         11 . A pharmaceutical composition comprising diethyl ether, ethyl acetate and n-butanol extracts from  Genista tenera  that inhibits the enzyme glucose-6-phosfatase, normalizing glucose levels.